1. Field of Invention
This invention refers to an ectoparasiticidal and antimycotic product for external use, which may be applied in human and veterinary medicine. More precisely, this invention consists of a copper oleate aqueous colloidal scatter.
2. Prior Art
The ectoparasiticidal products are drugs used in the treatment of skin infections caused by animal parasites. In humans, these pharmaceutical preparations are mainly insecticide and acaricide. The drugs currently available, used for the said purpose, are:
a) Lindane
The lindane or gamma benzene hexachloride has an insecticide and acaricide effect and is used for the treatment of the scabies. It is used at 1% in cream, lotion or shampoo. It is applied in fine layers on the neck and downwards and its effect may last from 4 to 8 or 12 hours depending on age and body area affected. A second application is made 5 days thereafter and another one ten days thereafter, following the birth cycle of the parasites. The lindane is used for the treatment of all pediculosis localizations. In general, only one application of lindane at 1% in shampoo, lotion or cream for 4 to 8 or 12 hours (according to the patient's age) is enough to eradicate the parasite, as it kills parasites and nits.
Unfortunately, the lindane has a quick transcutaneous absorption and high liposolubility, and it accumulates on the adipose tissue. It induces the mixed function oxidase system of the liver, it becomes debased slowly and lasts for a long time in the body. It acts on the presynaptic nervous terminals of the central nervous system, thus increasing the release of various neurotransmitters, and it may have consequences such as tremors, ataxia, convulsions and coma. It produces hepatoma in mice, although its carcinogenetic potential in human beings is doubtful.
b) Pirethrine
They are natural substances obtained from the pirethrum (chrysanthemus circerapiaefolium). The pirethoids are synthetic derivatives whose main examples are the permethrin and the decamethrin. Their efficacy is moderate since, although they are parasiticidal, they do not kill nits. They are presented as shampoo, lotion and cream. They are applied on the scalp for a time that varies from 10 minutes to 8 hours (depending on the patient's age) and then the nits affixed are taken out with a fine comb.
The permethrin acts on the membrane of the nervous cell of the parasite thus altering the sodium channel current which regulates the polarization of the membrane. This determines a late repolarization and the subsequent paralysis.
The decamethrin shares the same properties of the permethrin. The pirethrine and, in a higher proportion, the pirethoids, have marked allergenic properties (contact dermatitis and respiratory allergies).
c) Malathion
It is an irreversible organophosphorated anticholinesterasic insecticide. It is highly effective, but it is absorbed through the skin and it can cause a severe muscarinic intoxication if the directions for use are not strictly complied with, therefor its use is not advisable.
d) Benzyl benzoate
It is specially useful for the treatment of scabies and it is also used to treat pediculosis. It is irritating and frequently causes contact dermatitis, therefor its use is not advisable.
e) Diethiltoluamide
It is the most used insect repellent. Absorption through the skin is estimated between 10% and 15%. It produces allergic reactions and, in children, toxic encephalopathy, erythema and cutaneous ulcerations.
f) Copper
Copper is an oligoelement that takes part in many of the most important chemical reactions of the human body; among them, the ones related to erythropoyesis. The daily copper requirements are about 2.5 mg and they are easily covered with the diet. Any excess is easily eliminated by the body by means of a diminution of its gastrointestinal absorption by a complex homeostatic regulating mechanism.
The copper, used in the form of salts (oleate or sulfate) has antiseptic properties (sulfate), fungicide (sulfate and oleate) and parasiticidal (oleate). Copper salts have a not very powerful antiseptic activity, they rather have bacteriostatic effects when used in habitual concentrations.
The fungicide activity of the copper sulfate is specially used to destroy parasite mites of plants and, regarding the action mechanism, it is recognised that the copper cations precipitate the proteins and this is the reason for its local antiseptic effects, depending on the concentration used. The ectoparasiticidal activity is not clearly elucidated, but it is believed that the copper could act as a neurotoxic agent on the parasites. About 30% to 40% of the copper ingested is absorbed by the stomach and duodenum, followed by a quick transportation to the liver joined in a lax manner to the albumin. These complexes are dissociated in the hepatocytes membrane and the free copper is transferred inside the cells where it joins the apoceruloplasmine, and in this form it is excreted towards the serum.
The ceruloplasmine carries from 90 to 95% of the plasmatic copper and it is normally recycled in the liver, where it is degradated in the lysosomes thus releasing the copper, which is then excreted to the bile. The rest of the plasmatic copper is weakly joined to the albumin and is partly excreted to the bile. The quantity excreted by the kidney is very small as compared to the biliary excretion. The ingestion of excessive doses, for example 10 or more grams of copper sulfate causes symptoms derived from its local irritating activity at the gastrointestinal tract level; it produces nausea, vomiting, colic and diarrhea which may lead to collapse and shock. The ectoparaticidal formulae containing copper, known up to date, are mixtures of inflammable hydrocarbons, which contain a copper salt of a fatty acid dissolved in organic solvents. An apparent difficulty of these products is the high toxicity risk, since its formula favors cutaneous absorption and their permanence in the absorption place. On the other hand, due to is high irritating activity, contact of this product with the eyes, mucosas and open injuries must be avoided. Another adverse condition is the fact that it must be kept far from fire, due to its inflammability. Regarding its form of use, three or four spoonfuls of the mixture must be applied on the affected areas, leave overnight and remove with plenty of water and soap.